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Medication for treating senilism dementia and preparing technique

A technology for Alzheimer's disease and preparation technology, which is applied in the field of western medicine, can solve the problems of high toxic and side effects and insufficient drug efficacy, and achieve the effects of low toxic and side effects, wide application range, and simple and easy method

Inactive Publication Date: 2006-07-05
杨兴斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a medicine for treating Alzheimer's disease and its preparation process, so as to overcome the disadvantages of relatively large toxic and side effects and insufficient drug efficacy in the prior art.

Method used

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  • Medication for treating senilism dementia and preparing technique
  • Medication for treating senilism dementia and preparing technique
  • Medication for treating senilism dementia and preparing technique

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: see accompanying drawing, the synthesis of HA-T1 and HA-T2 compound

[0021] (1) Nicotinylation reaction: esterification reaction of huperzine A and nicotinic acid

[0022] Take 0.1 mmol of huperzine A, add anhydrous dichloromethane, stir in ice bath, add 0.4 mmol of nicotinic acid, 0.06 mmol of DMAP, 0.4 mmol of N, N-dicyclohexylcarbodiimide (DCC), and react under ice bath 3h, then reflux at 45°C for 8h. Stop the reaction, filter the reaction solution, wash with anhydrous dichloromethane, concentrate the filtrate, put it on a silica gel H column, and elute with the eluent (cyclohexane:ethyl acetate=4:1). The eluate was collected, plated, combined with the eluate containing the product, and vacuum-dried to obtain a sample, namely compound (A).

[0023] (2) Methanation reaction: Add compound (A) and an appropriate amount of anhydrous acetone into a reaction flask to form a suspension, stir, add excess methyl iodide dropwise, and stir for 48 hours in the d...

Embodiment 2

[0029] Embodiment 2: Synthesis of HA-T1 and HA-T2 compounds

[0030] (1) Nicotinylation reaction: alcoholysis reaction of huperzine A and nicotinyl chloride

[0031] Under anhydrous conditions and equipped with a drying device and a gas absorption device, the excess SOCl 2 Add it to the reaction bottle, cool it to about 0°C with an ice-water bath, stir, add 0.06mol of nicotinic acid, and drop in 5-7 drops of anhydrous DMF, slowly heat the oil bath to about 80°C, reflux for 3 hours, and evaporate SOCl under reduced pressure 2 , to obtain light yellow solid nicotinoyl chloride hydrochloride.

[0032] In an ice-salt bath, add 50 mL of acetone to the synthesized nicotinoyl chloride hydrochloride, add dropwise 30 mL of anhydrous triethylamine in acetone and 0.04 mol of Hup-A in acetone, react overnight at room temperature, filter, and concentrate the filtrate Add 90 mL of acetic acid aqueous solution (glacial acetic acid / water = 5 / 2), stir at room temperature for 2 h, add 25 mL o...

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PUM

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Abstract

A medicine for treating presenile dementia is just the HA-T1 which is the huperzine A derivative N-methyl-1,4-dihydropyridine-3-formate or the HA-T2 which is the huperzine A derivative N-methyl-1,2,5,6-tetrahydropyridine-3-formate. Its preparing process is also disclosed.

Description

Technical field: [0001] The invention relates to the technical field of western medicine, in particular to a medicine for treating Alzheimer's disease and a preparation process thereof. Background technique: [0002] Alzheimer's disease (AD), also known as Alzheimer's disease, is a neurodegenerative disease characterized by progressive memory and cognitive impairment and involving multiple etiological factors. The prevalence rate of people over 60 years old in my country is 3.4-3.9%, among them, the prevalence rate of AD in northern urban residents over 65 years old is 6.9%, which is close to that of Europe (6.4%) and Japan (7.0%). It is the fourth largest "killer" after cardiovascular disease, malignant tumor and stroke. With the aging of the world's population and the extension of the average life expectancy, AD has become an increasingly prominent social and medical problem, which will bring a heavy burden to the society and the medical care system. It is urgent to find e...

Claims

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Application Information

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IPC IPC(8): A61K31/439A61P25/28
Inventor 杨兴斌赵燕
Owner 杨兴斌
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